PI3K (p110alpha (E542K)/p85alpha) Kinase Enzyme Activity Assay Kit

Background Information:

The Kinase Enzyme Activity Assay Kit is a biochemical assay for the measurement of kinase inhibitors. The kit uses the HitHunter® assay technology and has been optimized for PI3K (p110alpha (E542K)/p85alpha) complex. All reagents are provided in the kit, including recombinant PI3K (p110alpha (E542K)/p85alpha) complex (Eurofins #14-782), substrate, ATP, detection reagents and assay plates. The COA that accompanies the kit details the optimal reaction conditions for the detection of kinase inhibitors. The kit includes sufficient material to run reactions for two 384-well assay plates. The E542K substitution is a somatic mutation in p110alpha that has been associated with tumours of the colon and brain. Combined in vitro and in vivo studies have shown that this mutation confers higher lipid kinase activity than wild type, and is able to induce oncogenic transformation. (Kang S. et al., PNAS, (2005); 102: 802-807 and Zhao J.J. et al., PNAS, (2005); 102:18443-18448).

Target Class:

Kinase

Family:

PI3/PI4-kinase

Sub Family:

Lipid kinase

Protein Name:

p110alpha/p85alpha complex

Protein Aliases:

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (p110alpha) / Phosphatidylinositol 3-kinase regulatory subunit alpha (p85alpha)

Accession Number:

GenBank U79143.1 (p110alpha); GenBank XM_043865.4 (p85alpha)

UniProt Number:

P42336 (p110alpha)/P27986 (p85

Gene Name:

PIK3CA (p110alpha)/PIK3R1 (p85alpha)

Gene ID:

5290 (p110alpha)/5295 (p85alph

Gene Aliases:

HMH; MCM; CCM4; CWS5; MCAP; PI3K; CLAPO; CLOVE; MCMTC; PI3K-alpha; p110-alpha (p110alpha) / p85; AGM

Target Species:

Human